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Page 1
Nav1.7 target modulation and efficacy can be measured in nonhuman primate assays.
Kraus RL, Zhao F, Pall PS, Zhou D, Vardigan JD, Danziger A, Li Y, Daley C, Ballard JE, Clements MK, Klein RM, Holahan MA, Greshock TJ, Kim RM, Layton ME, Burgey CS, Serra J, Henze DA, Houghton AK. Kraus RL, et al. Among authors: layton me. Sci Transl Med. 2021 May 19;13(594):eaay1050. doi: 10.1126/scitranslmed.aay1050. Sci Transl Med. 2021. PMID: 34011626
Discovery of selective, orally bioavailable, N-linked arylsulfonamide Nav1.7 inhibitors with pain efficacy in mice.
Roecker AJ, Egbertson M, Jones KLG, Gomez R, Kraus RL, Li Y, Koser AJ, Urban MO, Klein R, Clements M, Panigel J, Daley C, Wang J, Finger EN, Majercak J, Santarelli V, Gregan I, Cato M, Filzen T, Jovanovska A, Wang YH, Wang D, Joyce LA, Sherer EC, Peng X, Wang X, Sun H, Coleman PJ, Houghton AK, Layton ME. Roecker AJ, et al. Among authors: layton me. Bioorg Med Chem Lett. 2017 May 15;27(10):2087-2093. doi: 10.1016/j.bmcl.2017.03.085. Epub 2017 Mar 30. Bioorg Med Chem Lett. 2017. PMID: 28389149
Benzoxazolinone aryl sulfonamides as potent, selective Nav1.7 inhibitors with in vivo efficacy in a preclinical pain model.
Pero JE, Rossi MA, Lehman HDGF, Kelly MJ 3rd, Mulhearn JJ, Wolkenberg SE, Cato MJ, Clements MK, Daley CJ, Filzen T, Finger EN, Gregan Y, Henze DA, Jovanovska A, Klein R, Kraus RL, Li Y, Liang A, Majercak JM, Panigel J, Urban MO, Wang J, Wang YH, Houghton AK, Layton ME. Pero JE, et al. Among authors: layton me. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2683-2688. doi: 10.1016/j.bmcl.2017.04.040. Epub 2017 Apr 22. Bioorg Med Chem Lett. 2017. PMID: 28465103
Discovery of Arylsulfonamide Nav1.7 Inhibitors: IVIVC, MPO Methods, and Optimization of Selectivity Profile.
Roecker AJ, Layton ME, Pero JE, Kelly MJ 3rd, Greshock TJ, Kraus RL, Li Y, Klein R, Clements M, Daley C, Jovanovska A, Ballard JE, Wang D, Zhao F, Brunskill APJ, Peng X, Wang X, Sun H, Houghton AK, Burgey CS. Roecker AJ, et al. Among authors: layton me. ACS Med Chem Lett. 2021 Jun 1;12(6):1038-1049. doi: 10.1021/acsmedchemlett.1c00218. eCollection 2021 Jun 10. ACS Med Chem Lett. 2021. PMID: 34141090 Free PMC article.
Association of respiratory failure with inhibition of NaV1.6 in the phrenic nerve.
Klein RM, Layton ME, Regan H, Regan CP, Li Y, Filzen T, Cato M, Clements MK, Wang J, Sanoja R, Greshock TJ, Roecker AJ, Pero JE, Kim R, Burgey C, John CT, Wang YH, Bhandari N, Struyk A, Kraus RL, Henze DA, Houghton AK. Klein RM, et al. Among authors: layton me. Channels (Austin). 2022 Dec;16(1):230-243. doi: 10.1080/19336950.2022.2122309. Channels (Austin). 2022. PMID: 36239534 Free PMC article.
Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis.
Layton ME, Reif AJ, Hartingh TJ, Rodzinak K, Dudkin V, Wang C, Arrington K, Kelly MJ 3rd, Garbaccio RM, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Tang C, Kuo Y, Jacobson MA. Layton ME, et al. Bioorg Med Chem Lett. 2016 Feb 15;26(4):1260-4. doi: 10.1016/j.bmcl.2016.01.021. Epub 2016 Jan 11. Bioorg Med Chem Lett. 2016. PMID: 26810316
3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts.
Brnardic EJ, Fraley ME, Garbaccio RM, Layton ME, Sanders JM, Culberson C, Jacobson MA, Magliaro BC, Hutson PH, O'Brien JA, Huszar SL, Uslaner JM, Fillgrove KL, Tang C, Kuo Y, Sur SM, Hartman GD. Brnardic EJ, et al. Among authors: layton me. Bioorg Med Chem Lett. 2010 May 15;20(10):3129-33. doi: 10.1016/j.bmcl.2010.03.089. Epub 2010 Mar 31. Bioorg Med Chem Lett. 2010. PMID: 20409708
Discovery of 3-substituted aminocyclopentanes as potent and orally bioavailable NR2B subtype-selective NMDA antagonists.
Layton ME, Kelly MJ 3rd, Rodzinak KJ, Sanderson PE, Young SD, Bednar RA, Dilella AG, McDonald TP, Wang H, Mosser SD, Fay JF, Cunningham ME, Reiss DR, Fandozzi C, Trainor N, Liang A, Lis EV, Seabrook GR, Urban MO, Yergey J, Koblan KS. Layton ME, et al. ACS Chem Neurosci. 2011 Jul 20;2(7):352-62. doi: 10.1021/cn200013d. Epub 2011 Apr 15. ACS Chem Neurosci. 2011. PMID: 22816022 Free PMC article.
Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI.
Pero JE, Rossi MA, Kelly MJ 3rd, Lehman HD, Layton ME, Garbaccio RM, O'Brien JA, Magliaro BC, Uslaner JM, Huszar SL, Fillgrove KL, Tang C, Kuo Y, Joyce LA, Sherer EC, Jacobson MA. Pero JE, et al. Among authors: layton me. ACS Med Chem Lett. 2016 Jan 10;7(3):312-7. doi: 10.1021/acsmedchemlett.5b00459. eCollection 2016 Mar 10. ACS Med Chem Lett. 2016. PMID: 26985321 Free PMC article.
54 results